Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor

Discovery of a Bicyclic Peptidyl Pan-Ras Inhibitor

(2021) Marina Buyanova et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Frequency of Ras Mutations in Cancer

(2020) Ian A. Prior et al.   CANCER RESEARCH

Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer

(2020) Jay B. Fell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Drugging all RAS isoforms with one pocket

(2020) Dirk Kessler et al.   Future Medicinal Chemistry

Small-Molecule Inhibitors Directly Targeting KRAS as Anticancer Therapeutics

(2020) Hao Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Generation of KS-58 as the first K-Ras(G12D)-inhibitory peptide presenting anti-cancer activity in vivo

(2020) Kotaro Sakamoto et al.   Scientific Reports

Drugging an undruggable pocket on KRAS

(2019) Dirk Kessler et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity

(2019) Jude Canon et al.   NATURE

Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors

(2019) Brian A. Lanman et al.   JOURNAL OF MEDICINAL CHEMISTRY

The reactivity-driven biochemical mechanism of covalent KRASG12C inhibitors

(2018) Rasmus Hansen et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

The reactivity-driven biochemical mechanism of covalent KRASG12C inhibitors

(2018) Rasmus Hansen et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Lowering Lipophilicity by Adding Carbon: One-Carbon Bridges of Morpholines and Piperazines

(2018) Sébastien L. Degorce et al.   JOURNAL OF MEDICINAL CHEMISTRY

Salt Bridge in Ligand–Protein Complexes—Systematic Theoretical and Statistical Investigations

(2018) Rafał Kurczab et al.   Journal of Chemical Information and Modeling

Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity

(2018) Jay B. Fell et al.   ACS Medicinal Chemistry Letters

Crystal Structure of a Human K-Ras G12D Mutant in Complex with GDP and the Cyclic Inhibitory Peptide KRpep-2d

(2017) Satoshi Sogabe et al.   ACS Medicinal Chemistry Letters

Experimental and Theoretical Evaluation of the Ethynyl Moiety as a Halogen Bioisostere

(2015) Rainer Wilcken et al.   ACS Chemical Biology

Inhibition of Ras Signaling by Blocking Ras-Effector Interactions with Cyclic Peptides

(2015) Punit Upadhyaya et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Conformational restriction: an effective tactic in 'follow-on'-based drug discovery

(2014) Zengjun Fang et al.   Future Medicinal Chemistry

Drugging the undruggable RAS: Mission Possible?

(2014) Adrienne D. Cox et al.   NATURE REVIEWS DRUG DISCOVERY

Discovery of Small Molecules that Bind to K-Ras and Inhibit Sos-Mediated Activation

(2012) Qi Sun et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A Comprehensive Survey of Ras Mutations in Cancer

(2012) I. A. Prior et al.   CANCER RESEARCH

Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity

(2012) T. Maurer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Inhibition of Ras–effector interactions by cyclic peptides

(2012) Xianghong Wu et al.   MedChemComm